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Amdoal (Aripiprazolum, Aripiprazole) - neuroleptic.
The therapeutic effect of aripiprazole in schizophrenia is caused by a combination of partial agonistic activity on dopamine D2-and serotonin 5HT1A receptors and antagonistic activity against serotonin 5HT2-receptors.
Aripiprazole possesses high in vitro affinity for D2- and DZ-dopamine receptors, 5HT2A-5NT1a- and serotonin receptors and moderate affinity for the D4-dopamine, and 5NT2s- 5NT7-serotonin, Dl-adrenoceptors and H1 histamine receptors. Aripiprazole is also characterized by a moderate affinity for serotonin reuptake sites and the lack of affinity for muscarinic receptors. In animal experiments showed aripiprazole antagonism of dopaminergic hyperactivity and agonism at dopamine hypoactivity. The interaction not only with the dopamine and serotonin receptors explains some of the clinical effects of aripiprazole.
Precautions: cardiovascular disease (coronary heart disease, including myocardial infarction, chronic heart failure, conduction abnormalities, conditions that predispose to blood pressure reduction (dehydration, hypovolemia, taking antihypertensive drugs) because of the possibility of orthostatic hypotension, cerebrovascular disease, epilepsy, diseases in which seizures may develop, with the risk of aspiration pneumonia patients (due to the risk of disturbances in motor functions and esophageal aspiration) patients with an increased risk of hyperthermia, such as intense physical exercise, overheating, with receiving means m- anticholinergic activity, with dehydration (due to the ability of neuroleptics disrupt thermoregulation), patients with obesity, diabetes history, pregnancy.
Since the improvement of the patient in the treatment of neuroleptic drugs may require several days, patients should be closely monitored. The propensity to suicidal thoughts and attempts, characteristic of psychosis can occur in a short time after starting treatment or changing medication. Therefore, such patients should be carefully monitored.
Violations by the CCC. Aripiprazole should be used with caution in patients with cardiovascular disease (myocardial infarction or ischemic heart disease in history, heart failure, conduction abnormalities), cerebrovascular disorders, risk factors for hypotension (dehydration, hypovolemia, antihypertensive drugs), hypertension, including progressive and malignant .
In the application of neuroleptics may develop vein thrombosis. Since patients treated with antipsychotics may be predisposing factors for venous thromboembolism, should carry out a thorough examination of patients prior to treatment with aripiprazole and take preventive measures during treatment.
Conduction abnormalities. QT interval prolongation with aripiprazole rate corresponds to that of placebo. However, patients with a family history of QT interval prolongation should observe the same care in prescribing aripiprazole as the use of other antipsychotics.
Tardive Dyskinesia. The risk of developing tardive dyskinesia increases with the duration of treatment with neuroleptics, so you should reduce the dose or stop the drug when prompted during the treatment of symptoms of tardive dyskinesia. After discontinuation of these symptoms may temporarily worsen or even appear for the first time.
Neuroleptic malignant syndrome. When neuroleptic treatment may develop life-threatening neuroleptic malignant syndrome (hyperpyrexia, muscle rigidity, mental disorders and instability of the autonomic nervous system, including heart rate and unstable blood pressure, tachycardia, sweating, and arrhythmias). In addition, it is sometimes possible increase in CK activity, the emergence of myoglobinuria (rhabdomyolysis) and acute renal failure. In case of symptoms of neuroleptic malignant syndrome or unexplained fever medication should be discontinued.
Seizures. When aripiprazole cases of seizures have been observed. Therefore, caution should be exercised when treating patients with a history of seizures, or suffering from a disorder in which they can develop.
Elderly patients suffering from senile dementia. The drug is not approved for the treatment of senile psychoses, because It increases the risk of mortality and cerebrovascular complications.
Hyperglycemia and diabetes. Hyperglycemia (in some cases - marked with ketoacidosis), which can lead to hyperosmolar coma or death, has been noted in patients treated with atypical antipsychotics. Although the association between atypical antipsychotics and hyperglycemia remains unclear, patients diagnosed with diabetes requires regular monitoring of blood glucose when receiving atypical antipsychotics. In patients with risk factors for diabetes (obesity, diabetes mellitus family history) when taking hold of atypical neuroleptics necessary to determine the concentration of glucose in the blood at the beginning of the course and periodically during treatment. All patients treated with atypical antipsychotics, the constant control of hyperglycemia symptoms, including increased thirst, frequent urination, polyphagia, and weakness.
Hypersensitivity. Like other drugs, aripiprazole may cause hypersensitivity reactions.
Increased body weight. There was no effect of aripiprazole on weight gain.
Dysphagia. Admission antipsychotics including aripiprazole, causing esophageal dysmotility and aspiration. In patients at risk for aspiration pneumonia Aripiprazole and other antipsychotic drugs should be used with caution.
Lactose intolerance. The drug contains lactose, therefore it should not be taken in patients with rare hereditary disorders such as galactose intolerance, Lapp lactase deficiency or glucose-galactose syndrome malabsorption.
Effects on ability to drive vehicles and operate machinery. During treatment, care must be taken during the occupation activities that require high concentration and speed of psychomotor reactions.
Inside, 1 times a day, regardless of meals.
Schizophrenia. The recommended initial dose - 10-15 mg 1 time a day. Maintenance dose - 15 mg per day. The drug is effective in doses of 10 to 30 mg / day. Increasing the effectiveness of doses above 15 mg / day has not been proven, however, it may be required for some patients. The maximum daily dose should not exceed 30 mg.
Manic episodes in bipolar disorder. Initial dose - 15 mg / day as monotherapy, or in combination. Some patients may require a higher dose. The maximum daily dose should not exceed 30 mg.
Prevention of manic episodes in bipolar I disorder. For prophylaxis of manic episodes in patients who had previously taken aripiprazole alone or in combination, to continue the same medication dose. Correction of the daily dose, including the reduction is carried out in accordance with the condition of the patient.
Special patient groups
Patients with renal failure. Correction doses for the drug to patients with renal impairment is not required.
Patients with liver failure. Correction doses for the drug to patients with renal impairment is not required. However, in patients with severe hepatic impairment should be used with caution in the daily dose of 30 mg.
Patients older than 65 years. Dose adjustment is not required.
Influence of gender on the dosing regimen. The dosage regimen of the drug for patients of both sexes the same.
Dosages in concomitant therapy. With the simultaneous use of the drug Amdoal and potent inhibitors of CYP3A4 or CYP2D6 isoenzyme Amdoal dose of the drug should be reduced by 2 times. If you cancel isozymes CYP3A4 inhibitors of CYP2D6 or Amdoal dose should be increased. Amdoal should be applied without changing the dosage, if he is appointed as an adjunct therapy in patients with major depressive disorder. With the simultaneous use of the drug Amdoal and inducers of CYP3A4 Amdoal dose of the drug should be increased by 2 times. The additional increase in the dose of the drug Amdoal should be based on clinical indications. If you cancel inducers of CYP3A4 Amdoal dose of the drug should be reduced. In the appointment of several drugs that inhibit the CYP2D6 isoenzyme and of CYP3A4, should consider reducing the daily dose of the drug Amdoal.
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